• 제목/요약/키워드: new discovery

검색결과 905건 처리시간 0.039초

Toxicogenomics approaches in Toxicological Pathology

  • Shirai, Tomoyuki
    • 한국독성학회:학술대회논문집
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    • 한국독성학회 2002년도 Molecular and Cellular Response to Toxic Substances
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    • pp.116-116
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    • 2002
  • It is believed that cell and/or tissue toxicity is resulted from alterations in expression of many genes in response to environmental stresses or toxicants. New technology, such as DNA microarray analysis, can measure the expression of thousands of genes at a time providing the potential to accelerate discovery of toxicant pathways and specific gene targets.(omitted)

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Discovery of New Proteinase Inhibitor for the Treatment of Osteoporosis

  • 손문호
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 2001년도 춘계학술대회
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    • pp.89-99
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    • 2001
  • ■ Cathepsin K is a attractive target for selectively and efficiently modulating the osteoclastic bone resorption. ■ OST-1857 is a lead compound which is specifically targeted to cathepsin K and showed efficacy in TPTX rats. ■ OST-compounds are in process of the preclinical study, joined by Yuhan research center.

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An International Collaborative Program To Discover New Drugs from Tropical Biodiversity of Vietnam and Laos

  • Soejarto, Djaja D.;Pezzuto, John M.;Fong, Harry H.S.;Tan, Ghee Teng;Zhang, Hong Jie;Tamez, Pamela;Aydogmus, Zeynep;Chien, Nguyen Quyet;Franzblau, Scott G.;Gyllenhaal, Charlotte;Regalado, Jacinto C.;Hung, Nguyen Van;Hoang, Vu Dinh;Hiep, Nguyen Tien;Xuan, Le Thi;Hai, Nong Van;Cuong, Nguyen Manh;Bich, Truong Quang;Loc, Phan Ke;Vu, Bui Minh;Southavong, Boun Hoong
    • Natural Product Sciences
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    • 제8권1호
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    • pp.1-15
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    • 2002
  • An International Cooperative Biodiversity Group (ICBG) program based at the University of Illinois at Chicago initiated its activities in 1998, with the following specific objectives: (a) inventory and conservation of of plants of Cuc Phuong National Park in Vietnam and of medicinal plants of Laos; (b) drug discovery (and development) based on plants of Vietnam and Laos; and (c) economic development of communities participating in the ICBG project both in Vietnam and Laos. Member-institutions and an industrial partner of this ICBG are bound by a Memorandum of Agreement that recognizes property and intellectual property rights, prior informed consent for access to genetic resources and to indigenous knowledge, the sharing of benefits that may arise from the drug discovery effort, and the provision of short-term and long-term benefits to host country institutions and communities. The drug discovery effort is targeted to the search for agents for therapies against malaria (antimalarial assay of plant extracts, using Plasmodium falciparum clones), AIDS (anti-HIV-l activity using HOG.R5 reporter cell line (through transactivation of the green fluorescent protein/GFP gene), cancer (screening of plant extracts in 6 human tumor cell lines - KB, Col-2, LU-l, LNCaP, HUVEC, hTert-RPEl), tuberculosis (screening of extracts in the microplate Alamar Blue assay against Mycobacterium tuberculosis $H_{37}Ra\;and\;H_{37}Rv),$ all performed at UIC, and CNS-related diseases (with special focus on Alzheimer's disease, pain and rheumatoid arthritis, and asthma), peformed at Glaxo Smith Kline (UK). Source plants were selected based on two approaches: biodiversity-based (plants of Cuc Phuong National Park) and ethnobotany-based (medicinal plants of Cuc Phuong National Park in Vietnam and medicinal plants of Laos). At mc, as of July, 2001, active leads had been identified in the anti-HIV, anticancer, antimalarial, and anti- TB assay, after the screening of more than 800 extracts. At least 25 biologically active compounds have been isolated, 13 of which are new with anti-HIV activity, and 3 also new with antimalarial activity. At GSK of 21 plant samples with a history of use to treat CNS-related diseases tested to date, a number showed activity against one or more of the CNS assay targets used, but no new compounds have been isolated. The results of the drug discovery effort to date indicate that tropical plant diversity of Vietnam and Laos unquestionably harbors biologically active chemical entities, which, through further research, may eventually yield candidates for drug development. Although the substantial monetary benefit of the drug discovery process (royalties) is a long way off, the UIC ICBG program provides direct and real-term benefits to host country institutions and communities.

워크플로우 소셜네트워크 인텔리전스 발견 알고리즘 (A Workflow-based Social Network Intelligence Discovery Algorithm)

  • 김광훈
    • 인터넷정보학회논문지
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    • 제13권2호
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    • pp.73-86
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    • 2012
  • 본 논문에서는 워크플로우 소셜네트워크 인텔리전스의 발견 알고리즘을 제안한다. 즉, 워크플로우 인텔리전스 (또는 비즈니스 프로세스 인텔리전스) 기술은 워크플로우 모델들과 그의 실행이력으로부터 일련의 인텔리전스를 발견, 분석, 모니터링 및 제어, 그리고 예측하는 세부기법들로 구성되는데, 본 논문에서는 워크플로우 모델과 그의 실행을 기반으로 형성되는 수행자들간의 협업 인텔리전스를 "워크플로우 소셜네크워크 인텔리전스"라고 정의하고, 그의 발견기법인 정보제어넷(ICN, Information Control Net)기반 워크플로우 소셜네트워크 인텔리전스 발견 알고리즘을 제안한다. 특히, 제안한 알고리즘의 적용 사례를 통해 특정 워크플로우 모델로부터 해당 워크플로우 소셜네트워크 인텔리전스를 성공적으로 생성할 수 있음을 증명하므로서 본 논문에서 제안한 알고리즘의 정확성 및 적합성을 검증한다.

Purification and Characterization of HCV RNA-dependent RNA Polymerase from Korean Genotype 1b Isolate: Implications for Discovery of HCV Polymerase Inhibitors

  • Kim, Jeong-Min;Lee, Mi-Kyoung;Kim, Yong-Zu
    • Bulletin of the Korean Chemical Society
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    • 제26권2호
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    • pp.285-291
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    • 2005
  • The nonstructural protein 5B (NS5B) of hepatitis C virus (HCV) is the viral RNA-dependent RNA polymerase (RdRp), which is the essential catalytic enzyme for the viral replication and is an appealing target for the development of new therapeutic agents against HCV infection. A small amount of serum from a single patient with hepatitis C was used to get the genome of a Korean HCV isolate. Sequence analysis of NS5B 1701 nucleotides showed the genotype of a Korean isolate to be subtype 1b. The soluble recombinant HCV NS5B polymerase lacking the C-terminal 24 amino acids was expressed and purified to homogeneity. With the highly purified NS5B protein, we established in vitro systems for RdRp activity to identify potential polymerase inhibitors. The rhodanine family compounds were found to be potent and specific inhibitors of NS5B from high throughput screening (HTS) assay utilizing the scintillation proximity assay (SPA) system. The binding mode of an inhibitor was analyzed by measuring various kinetic parameters. Lineweaver-Burk plots of the inhibitor suggested it binds not to the active site of NS5B polymerase, but to an allosteric site of the enzyme. The activity of NS5B in in vitro polymerase reactions with homopolymeric RNA requires interaction with multiple substrates that include a template/primer and ribonucleotide triphosphate. Steady-state kinetic parameter, such as Km, was determined for the ribonucleotide triphosphate. One of compounds found interacts directly with the viral polymerase and inhibits RNA synthesis in a manner noncompetitively with respect to UTP. Furthermore, we also investigated the ability of the compound to inhibit NS5B-directed viral RNA replication using the Huh7 cell-based HCV replicon system. The investigation is potentially very useful for the utility of such compounds as anti-hepatitic agents.

상이한 특성을 갖는 아이템 그룹에 대한 가중 연관 규칙 탐사 (Weighted Association Rule Discovery for Item Groups with Different Properties)

  • 김정자;정희택
    • 한국정보통신학회논문지
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    • 제8권6호
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    • pp.1284-1290
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    • 2004
  • 장바구니 분석에서, 가중 연관 규칙 탐사는 특정 상품에 대한 아이템의 중요도를 반영함으로써 더 많은 이익을 주는 정보를 규칙으로 탐사하였다. 그러나 트랜잭션을 구성하는 아이템들이 한 개 이상의 서로 다른 그룹으로 나누어진다면, 각 그룹의 특성을 반영하는 서로 다른 측정 방법으로 평가되어야 하므로 기존의 가중연관규칙 탐사 방법을 적용할 수가 없다. 본 논문에서는 이를 해결하기 위해서 가중 연관 규칙의 새로운 탐사 방법을 제안하였다. 먼저 각 아이템들은 유사한 특성에 따라 서브 그룹으로 나누고, 아이템 중요도(아이템 가중치)는 서브 그룹에 포함된 아이템들 단위로 계산한다 이때 적용되는 여러 가중 인자들은 아이템의 특성을 반영하는 아이템 그룹별로 재 정의하였다. 제안하는 방법은 네트워크 보안 데이터에 적용하여 위험을 일으키는 요소에 대한 위험 규칙 집합을 생성함으로써 네트워크 위험관리의 정성평가와, 규칙 생성 시 적용된 가중치와 같은 여러 통계인자들에 의해서 위험도를 계산함으로써 정량평가를 가능하게 하였다. 또한 데이터 아이템들이 상이하게 구별될 수 있는 특성을 만족하는 마켓 데이터의 새로운 응용분야에 넓게 적용될 수 있다.

Ultra-fast Generic LC-MS/MS Method for High-Throughput Quantification in Drug Discovery

  • Kim, So-Hee;Yoo, Hye Hyun;Cha, Eun-Ju;Jeong, Eun Sook;Kim, Ho Jun;Kim, Dong Hyun;Lee, Jaeick
    • Mass Spectrometry Letters
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    • 제4권3호
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    • pp.47-50
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    • 2013
  • An ultra-fast generic LC-MS/MS method was developed for high-throughput quantification of discovery pharmacokinetic (PK) samples and its reliability was verified. The method involves a simple protein precipitation for sample preparation and the analysis by ultra-fast generic LC-MS/MS with the ballistic gradient program and selected reaction monitoring (SRM) mode. Approximately 290 new chemical entities (NCEs) (over 10,000 samples) from 5 therapeutic programs were analyzed. The calibration curves showed good linearity in the concentration range of 1, 2 or 5 to 2000 ng/mL. No significant ion suppression was observed in the elution region of all the NCEs. When approximately 300 plasma samples were continuously analyzed, the peak area of internal standard was constant and reproducible. In the repeated analysis of samples, the plasma concentrations and the area under the curve (AUC) were consistent with the results from the first analysis. These results showed that the present ultra-fast generic LC-MS/MS method is reliable in terms of selectivity, sensitivity, and reproducibility and could be useful for high-throughput quantification and other bioanalysis in drug discovery.

Zirconium(IV) Chloride - Catalysed Reaction of Indoles: An Expeditious Synthesis of Bis(indolyl)methanes

  • Nagawade, Rahul R.;Shinde, Devanand B.
    • Bulletin of the Korean Chemical Society
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    • 제26권12호
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    • pp.1962-1964
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    • 2005
  • Zirconium(IV) chloride is found to be an efficient catalyst for the electrophilic addition reaction of indole with aldehydes/ketones to afford the corresponding bis(indolyl methanes in good yields. The remarkable features of this new procedure are high conversions, shorter reaction times, cleaner reaction profiles and simple experimental and work-up procedures.

Control of Influenza: Live Vaccine Development

  • Seong, Baik-Lin
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.149-150
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    • 2002
  • Despite various efforts on improving vaccines and antivirals, influenza epidemics continue to afflict many people, causing widespread morbidity and mortality in the young and the elderly. Since the discovery of the unusual 'cap-stealing'mechanism of transcription, significant advances were made on molecular aspects of influenza gene regulation. This provides new insights for developing new antiviral compounds. Reverse genetic technologies have also been advanced for generating recombinant chimeric viruses suitable for designing live vaccine. (omitted)

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Self-tuning Robust Regression Estimation

  • Park, You-Sung;Lee, Dong-Hee
    • 한국통계학회:학술대회논문집
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    • 한국통계학회 2003년도 추계 학술발표회 논문집
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    • pp.257-262
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    • 2003
  • We introduce a new robust regression estimator, self-tuning regression estimator. Various robust estimators have been developed with discovery for theories and applications since Huber introduced M-estimator at 1960's. We start by announcing various robust estimators and their properties, including their advantages and disadvantages, and furthermore, new estimator overcomes drawbacks of other robust regression estimators, such as ineffective computation on preserving robustness properties.

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